Table 3

Kinetic parameters for 7-ethoxy-4-trifluoromethylcoumarin O-deethylation by microsomes from COS-1 cells expressing wild-type and variant CYP2B6s

VariantKmVmaxVmax
ProteinP450ProteinP450
μM pmol/min/mg protein pmol/min/pmol CYP2B6 μl/min/mg protein μl/min/pmol CYP2B6
CYP2B6.15.50  ± 0.449.97  ± 1.703.93  ± 0.451.91  ± 0.430.72  ± 0.07
CYP2B6.26.28  ± 0.518.85  ± 2.546.52  ± 0.771.42  ± 0.361.04  ± 0.08
CYP2B6.36.36  ± 0.729.24  ± 1.936.31  ± 0.821.47  ± 0.321.01  ± 0.12
CYP2B6.46.01  ± 0.5512.7  ± 2.457.72  ± 1.04** 2.10  ± 0.271.30  ± 0.20**
CYP2B6.55.71  ± 0.199.59  ± 2.076.60  ± 0.201.72  ± 0.421.16  ± 0.02*
CYP2B6.67.71  ± 0.29* 17.7  ± 4.1310.3  ± 0.54** 2.31  ± 0.521.34  ± 0.07**
CYP2B6.77.53  ± 0.5414.7  ± 4.169.70  ± 0.72** 2.01  ± 0.601.31  ± 0.14**

Each value represents the mean ± S.E. of four separate experiments derived from independent preparations.

  • 3-178 p < 0.05, ∗∗ p < 0.01 versus CYP2B6.1.